5-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]thiophene-2-sulfonamide → 5-{5-chloro-4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl}thiophene-2-sulfonamide

Participants

Reaction Steps

Using 2-bromo-5-chloro-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidin-4-amine as starting material, following same procedure as described in Compound 50, the HCl salt of 5-(5-chloro-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrimidin-2-yl)thiophene-2-sulfonamide (Compound 42) was prepared (92.7 mg, 33.4%). LC-MS (m/z)=397.0 [M+H]+; 1H NMR (400 MHz, DMSO-d6): 0.78-0.79 (m, 2H), 1.00-1.02 (m, 2H), 1.97-1.99 (m, 1H), 6.42 (s, 1H), 7.59 (d, J=4.4 Hz, 1H), 7.78 (d, J=3.6 Hz, 1H), 7.84 (s, 2H), 8.50 (s, 1H), 9.65 (s, 1H).

Provenance & Evidence